Silicon Or Phosphorus Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 540/487)
  • Patent number: 9102704
    Abstract: A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; —CH2—O—C(?O)Me; R8 is OProto, where Proto is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) C(?O)—ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) —CH2—O—C(?O)RC2, where RC2 is methyl or phenyl; (iii) CH2—O—Si—(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) C(—YRC3)(—YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: August 11, 2015
    Assignee: SPIROGEN SARL
    Inventors: Philip Wilson Howard, Arnaud Tiberghien
  • Patent number: 8841257
    Abstract: Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: September 23, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventors: John S. McMurray, Pijus K. Mandal, Warren S. Liao, Fredika Robertson, Xiaomin Chen, Ramesh Rajaopal, Zhiyong Ren
  • Publication number: 20140275522
    Abstract: A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; —CH2—O—C(?O)Me; R8 is OProto, where Proto is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) C(?O)—ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) —CH2—O—C(?O)RC2, where RC2 is methyl or phenyl; (iii) CH2—O—Si—(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) C(—YRC3)(—YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 18, 2014
    Applicant: SPIROGEN SÁRL
    Inventors: Philip Wilson Howard, Arnaud Tiberghien
  • Publication number: 20140087992
    Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.
    Type: Application
    Filed: September 20, 2013
    Publication date: March 27, 2014
    Inventors: Ashvinikumar V. Gavai, George V. DeLucca, Daniel O'Malley, Patrice Gill, Claude A. Quesnelle, Brian E. Fink, Yufen Zhao, Francis Y. Lee
  • Publication number: 20130137659
    Abstract: Provided herein are compounds of formula (I):
    Type: Application
    Filed: January 25, 2013
    Publication date: May 30, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Publication number: 20130059800
    Abstract: Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.
    Type: Application
    Filed: April 15, 2011
    Publication date: March 7, 2013
    Applicants: SEATTLE GENETICS INC., SPIROGEN DEVELOPMENTS SÀRL
    Inventors: Philip Wilson Howard, Luke Masterson, Arnaud Tiberghien, Scott Jeffrey, Patrick Burke, Peter Senter
  • Publication number: 20130053347
    Abstract: The present invention relates to the biology and mechanism of action of the naturally occurring compound Narciclasine, especially as an anti-cancer agent for brain tumors. The invention provides new insights on the target molecule of Amaryllidaceae isocarbostyril derivatives as for example Narciclasine and provides new prodrugs of these Amaryllidceae isocabostyril constituents for treating cancer, specifically cancers or tumors located in the brain.
    Type: Application
    Filed: May 3, 2010
    Publication date: February 28, 2013
    Applicant: Universite Libre de Bruxelles
    Inventors: Veronique Mathieu, Gwendoline Van Goietsenoven, Jacques Dubois, Florence Lefranc-Kiss, Laurent Ingrassia, Robert Kiss
  • Patent number: 8378094
    Abstract: Coupling-initiator compounds are described that include a silicon-containing coupling moiety and at least one polymerization initiator moiety. The coupling moiety may be linked to the at least one polymerization initiator moiety by at least one linking moiety. The coupling moiety is capable of coupling the compound to a substrate, while the one or more polymerization initiator moieties are capable of initiating a polymerization of a monomer under polymerization conditions. The coupling-initiator compounds may be included in fiber reinforced polymer composites, where the compounds are coupled to the fibers in the composites and participate in the polymerization of the surrounding polymer.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 19, 2013
    Assignee: Johns Manville
    Inventors: Kiarash Alavi Shooshtari, Jawed Asrar, Rajappa Tadepalli, Thomas Burghardt, Klaus Friedrich Gleich
  • Publication number: 20120097935
    Abstract: The present invention relates to novel compounds of the formula (I) wherein R1 and R1? independently of each other are H or a substituent, halogen or SiR6R4R5; R2 and R2? may be the same or different and are selected from C1-C25alkyl, C3-C12-cycloalkyl, C2-C25alkenyl, C2-C25alkynyl, C4-C25aryl, C5-C25alkylaryl or C5-C25aralkyl, each of which is unsubstituted or substituted, and under conditions as defined in claim 1, R2 and/or R2? may also be halogen or hydrogen; X is a divalent linking group selected from formula (Ia) and formula (Ib); Y and Y? independently are selected from formula (Ic), formula (Id), formula (Ie), formula (If), formula (Ig); n and p independently range from 0 to 6; where further symbols are as defined in claim 1, and to corresponding oligomers and (co)polymers. The compounds according to the invention are useful as semiconductors and have excellent solubility in organic solvents and excellent film-forming properties.
    Type: Application
    Filed: May 21, 2010
    Publication date: April 26, 2012
    Applicant: BASF SE
    Inventors: Hans Jürg Kirner, Natalia Chebotareva, Olivier Frédéric Aebischer
  • Publication number: 20120035114
    Abstract: Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.
    Type: Application
    Filed: April 9, 2010
    Publication date: February 9, 2012
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: John S. McMurray, Pijus K. Mandal, Warren S. Liao, Fredika Robertson, Xiaomin Chen, Ramesh Rajaopal, Zhiyong Ren
  • Publication number: 20120006358
    Abstract: The invention relates to machine dishwashing agents containing specific polycarbonate-, polyurethane-, and/or polyurea-polyorganosiloxane compounds or precursor compounds thereof of the reactive cyclic carbonate and urea type which help to avoid the formation of water spots and filming after the use of the agents and accelerate the drying of dishes.
    Type: Application
    Filed: September 20, 2011
    Publication date: January 12, 2012
    Applicant: Henkel AG & Co. KGaA
    Inventors: Nadine Warkotsch, Marc-Steffen Schiedel, Johannes Zipfel, Arnd Kessler
  • Patent number: 8080544
    Abstract: Disclosed are prodrug compounds of formula (I) (wherein variables R1 and R2 are as described herein) which are analogues of an antagonist of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: February 4, 2009
    Date of Patent: December 20, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Valentino J. Stella
  • Publication number: 20110082111
    Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: December 7, 2010
    Publication date: April 7, 2011
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Sheldon X. Cao, Victoria Feher, Takashi Ichikawa, Benjamin Jones, Stephen W. KALDOR, Andre A. KIRYANOV, Betty Lam, Yan Liu, Christopher McBride, Srinivasa Reddy Natala, Zhe Nie, Jeffrey A. Stafford
  • Publication number: 20110062426
    Abstract: A process for the preparation of a substituted 2,2?-dithiophene is described, which process comprises the steps (a), (c) and optional steps (b) and (d): a reaction of a compound of the formula: with a suitable lithium organic compound, preferably Li-alkyl or Li-alkylamide; b) optional exchange of lithium against another metal selected from Mg1 Zn and Cu; c) reaction of the metallated intermediate obtained in step (a) or (b) with a suitable electrophil, which is CO2 or an aldehyde (addition reaction), or a compound Y?—R17 or Y?—R18-Z (substitution reaction), where R17 and R18 are as defined in claim 1; and optionally d) modification of the product obtained in step (c), e.g. by introducing one or more conjugating moieties Y ring closure between suitable monovalent residues R17, exchange or extension of functional groups or substituents such as addition to carbonyl or substitution of carbonyl in R17 or R18.
    Type: Application
    Filed: March 6, 2009
    Publication date: March 17, 2011
    Applicant: BASF SE
    Inventors: Hans Jurg Kirner, Frank Bienewald, Jean Charles Flores, Oliver Frédéric Aebischer
  • Publication number: 20100298269
    Abstract: Disclosed are prodrug compounds of formula (I) (wherein variables R1 and R2 are as described herein) which are analogues of an antagonist of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: February 4, 2009
    Publication date: November 25, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Valentino J. Stella
  • Publication number: 20100280239
    Abstract: Coupling-initiator compounds are described that include a silicon-containing coupling moiety and at least one polymerization initiator moiety. The coupling moiety may be linked to the at least one polymerization initiator moiety by at least one linking moiety. The coupling moiety is capable of coupling the compound to a substrate, while the one or more polymerization initiator moieties are capable of initiating a polymerization of a monomer under polymerization conditions. The coupling-initiator compounds may be included in fiber reinforced polymer composites, where the compounds are coupled to the fibers in the composites and participate in the polymerization of the surrounding polymer.
    Type: Application
    Filed: March 15, 2010
    Publication date: November 4, 2010
    Inventors: Kiarash Alavi Shooshtari, Jawed Asrar, Rajappa Tadepalli, Thomas Burghardt, Klaus Friedrich Gleich
  • Publication number: 20090005528
    Abstract: In one aspect, the invention relates to silicon-based prepolymers. The disclosed prepolymers exhibit satisfactory solubility in aqueous solutions or hydrophilic solutions and can overcome undesirable shrinkage, expansion, and related problems possessed by conventional silicone monomers and related conventional polymerization techniques by producing hydrogels from a crosslinkable prepolymer. Also disclosed are polymers and molded articles produced from the disclosed prepolymers, which attain a satisfactory oxygen permeability. Also disclosed are methods for producing the disclosed prepolymers. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 29, 2007
    Publication date: January 1, 2009
    Inventors: Kazuhiko Fujisawa, Mitsuru Yokota, Masataka Nakamura
  • Publication number: 20080318905
    Abstract: Prodrugs of parent drugs and methods of making and using the same are described. The prodrugs comprise an amine-containing parent drug moiety and a prodrug moiety, such as methoxyphosphonic acid or ethoxyphosphonic acid. The prodrugs may be employed in therapy for the treatment of various indications, such as pain, and in methods of decreasing the abuse potential of abuse-prone drugs and/or delaying the onset of parent drug activity and/or prolonging parent drug activity as compared to administration of a parent drug.
    Type: Application
    Filed: December 5, 2007
    Publication date: December 25, 2008
    Inventors: Naweed Muhammad, Keith R. Bley
  • Patent number: 7368444
    Abstract: The present invention relates to the compound presented by formula (I) (wherein all symbols in formula (I) are the same mean as the description shown in the specification.), mitocondorial benzogeazepin receptor (MBR) antagonist comprising the compound, the preventive and/or treatment medicine against diseases caused by stress of which an active ingredient is the compound. Since the compound represented by formula (I) has MBR antagonistic activity, and controls the production of neurosteroid, it is useful as the preventive and/or treatment medicine against diseases caused by stress.
    Type: Grant
    Filed: February 13, 2003
    Date of Patent: May 6, 2008
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Takuya Seko, Seishi Katsumata, Masashi Kato, Jun-ichiro Manako, Kazuyuki Ohmoto
  • Patent number: 6686350
    Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
    Type: Grant
    Filed: January 25, 1999
    Date of Patent: February 3, 2004
    Assignee: Biogen, Inc.
    Inventors: Zhongli Zheng, Carol L. Ensinger, Steven P. Adams
  • Publication number: 20030176398
    Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
    Type: Application
    Filed: June 11, 2002
    Publication date: September 18, 2003
    Inventors: Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fayang G. Qiu, Fenmei Yao, Jia-Ning Xiang, Ian R. Ollmann
  • Publication number: 20030149262
    Abstract: The present invention describes novel compounds of the formula:
    Type: Application
    Filed: November 26, 2002
    Publication date: August 7, 2003
    Inventors: Edward H. Cheesman, Michael Sworin
  • Publication number: 20030139377
    Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections: 1
    Type: Application
    Filed: November 12, 2002
    Publication date: July 24, 2003
    Applicant: SmithKline Beecham Corporation
    Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld
  • Publication number: 20030134827
    Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1
    Type: Application
    Filed: March 12, 2002
    Publication date: July 17, 2003
    Inventors: Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie
  • Patent number: 6576760
    Abstract: Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the polyamines except two being fully substituted and the remaining two bearing one H atom each, are cyclized by reaction with a bridging agent that contains two sites that each bear a reactive group capable of undergoing a nucleophilic attack by one of the two N-H groups on the polyamine. Unlike the prior art, cyclization occurs in preference over polymerization of the polyamine, even in reaction mixtures in which the polyamine is at high concentration. A process is also disclosed whereby linear polyamines in which the terminal amine groups are primary amines are substituted with methylenephosphonate ester groups, with one such substituent on each nitrogen atom of the polyamine.
    Type: Grant
    Filed: January 11, 2001
    Date of Patent: June 10, 2003
    Assignee: Chelator LLC
    Inventors: Harry S. Winchell, Rosa L. Cyjon, Joseph Y. Klein, Elliot D. Simhon, Ofer Klein, Haim Zaklad
  • Publication number: 20030092677
    Abstract: The present invention is a compound of formula 1
    Type: Application
    Filed: November 20, 2002
    Publication date: May 15, 2003
    Inventors: Geo Adam, Alaxander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Patent number: 6521613
    Abstract: Compounds, compositions and methods are disclosed useful for enhancing penetration of a pharmacologically active substances across skin or tissue membranes. Compounds for use in such compositions and methods are highly water-soluble N-substituted polyalkylene oxide derivatives of cyclic amides. A compound of the invention has the structural formula: wherein m is an integer from 2 to about 6, n is an integer from 1 to about 8, and R is hydrogen, trimethylsilyl or lower alkyl.
    Type: Grant
    Filed: April 10, 2001
    Date of Patent: February 18, 2003
    Assignee: Allergan, Inc.
    Inventor: Gary Ewing
  • Patent number: 6503898
    Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.
    Type: Grant
    Filed: July 10, 1998
    Date of Patent: January 7, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Patrick Yuk-Sun Lam, Prabhakar Kondaji Jadhav, Charles Joseph Eyermann, Carl Nicholas Hodge, George Vincent De Lucca, James David Rodgers
  • Patent number: 6399598
    Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptacle salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: June 4, 2002
    Assignee: The Procter & Gamble Company
    Inventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
  • Patent number: 6372735
    Abstract: Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereof. The compounds are useful as antiallergic agents and exhibit excellent bioavailability.
    Type: Grant
    Filed: March 29, 2000
    Date of Patent: April 16, 2002
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Yasuo Ohtsuka, Toshio Nishizuka, Sohjiro Shiokawa, Seiji Tsutsumi, Mami Kawaguchi, Hideo Kitagawa, Hiromi Takata, Takashi Shishikura, Toyoaki Ishikura, Kenichi Fushihara, Yumiko Okada, Sachiko Miyamoto, Maki Shiobara
  • Publication number: 20020042398
    Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1
    Type: Application
    Filed: July 10, 2001
    Publication date: April 11, 2002
    Inventors: Thomas P. Maduskuie, Jingwu Duan, Stephen E. Mercer
  • Publication number: 20020042508
    Abstract: The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.
    Type: Application
    Filed: September 20, 2001
    Publication date: April 11, 2002
    Inventors: Neil Warren Boaz, Sheryl Davis Debenham
  • Patent number: 6344560
    Abstract: A nitroaromatic compound is used to enhance the solubility of a nitroxyl compound in an aromatic hydrocarbon solvent.
    Type: Grant
    Filed: May 3, 2000
    Date of Patent: February 5, 2002
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Brendan J. Geelan, Brigitte Benage, Gerald J. Abruscato, Kirk A. Schlup, Ruben S. Grewal, Andrew J. Eisenstein
  • Publication number: 20020004494
    Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1
    Type: Application
    Filed: May 22, 2001
    Publication date: January 10, 2002
    Inventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
  • Patent number: 6323195
    Abstract: This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12alkylcarbonyl, (C1-C12)alkoxycarbonyl, mono(C1-C12)alkylaminocarbonyl, or di(C1-C12)alkylaminocarbonyl; R2 is hydrogen, (C3-C12)alkenylcarbonyloxy, (C3-C12)cycloalkylcarbonyloxy, (C3-C12)cycloalkyl(C1-C12)alkylcarbonyloxy, oxygen containing heterocycloxy, oxygen containing heterocyclylcarbonyloxy, sulfur containing heterocyclyloxy, sulfur containing heterocyclylcarbonyloxy, nitrogen containing hetercyclyloxy, nitrogen containing heterocyclylcarbonyloxy, haloalkylsulfonyloxy, (C1-C6)alkylsilyloxy; R3 is hydrogen, halo or (C1-C4)alkyl; R4 is hydrogen or (C1-C6)alkyl; with the proviso that R1 and R2 are not both hydrogen when R3 and R4 are hydrogen; all geometric, and optical stereoisomers thereof, or a pharmaceutically acceptable addition salt thereof; which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing t
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: November 27, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
  • Patent number: 6262222
    Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: July 17, 2001
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
  • Patent number: 6207663
    Abstract: Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I A—B—D—E—F—G   (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: October 5, 1999
    Date of Patent: March 27, 2001
    Assignees: Hoechst Atkiengesellschaft, Genentech, Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel LeFrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 6130231
    Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: October 10, 2000
    Assignee: DuPont Pharmaceuticals
    Inventors: John Wityak, Aleksandra Ewa Tobin
  • Patent number: 6121258
    Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: September 19, 2000
    Assignee: The Procter & Gamble Company
    Inventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
  • Patent number: 6114522
    Abstract: A process for producing 4-substituted-3-halogeno-1,4-benzoxazepin derivative or the salt thereof comprising: deprotonizing a benzoxazepine derivative having the formula (II): ##STR1## with a base; and then, reacting the deprotonized product with a phosphate halide to produce an intermediate having the formula (IV): ##STR2## and then, reacting the resultant intermediate (IV) with a reagent selected from (i) a complex of a phosphine with chlorine or bromine, (ii) a phosphine and a chlorine gas or liquid bromine, (iii) a phosphine and tetrachloromethane or tetrabromomethane, or (iv) a halogenated phosphite ester to produce a 4-substituted-3-halogeno-1,4-benzoxazepine derivative having the formula (I) ##STR3## wherein X indicates a chlorine atom or a bromine atom, or its salt.
    Type: Grant
    Filed: November 24, 1999
    Date of Patent: September 5, 2000
    Assignee: Suntory Limited
    Inventors: Kastuhide Kamei, Noriko Maeda, Toshio Tatsuoka
  • Patent number: 6051678
    Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.
    Type: Grant
    Filed: March 13, 1997
    Date of Patent: April 18, 2000
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
  • Patent number: 6034215
    Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
    Type: Grant
    Filed: October 14, 1997
    Date of Patent: March 7, 2000
    Assignee: Corvas International, Inc.
    Inventors: Joseph Edward Semple, Robert John Ardecky, Ruth Foelsche Nutt, William Charles Ripka, David C. Rowley, Marguerita S. L. Lim-Wilby, Terence Kevin Brunck
  • Patent number: 5994537
    Abstract: Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.
    Type: Grant
    Filed: February 14, 1998
    Date of Patent: November 30, 1999
    Assignee: Bristol-Myers Squibb Co.
    Inventor: Jeffrey A. Robl
  • Patent number: 5981511
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: March 5, 1997
    Date of Patent: November 9, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Rolando E. Gapud, Timothy J. Hagen, Ann E. Hallinan, Donald W. Hansen, Jr., Robert E. Manning, Suzanne Metz, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, R. Keith Webber
  • Patent number: 5955606
    Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: September 21, 1999
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
  • Patent number: 5952462
    Abstract: Antigens capable of eliciting antibodies which can catalyze chemical reactions, in particular, the cleavage or formation of a peptide linkage, comprising a hapten or a hapten and a suitable carrier molecule are disclosed. Haptens include, among others, silicon and boron containing compounds. Antibodies which are catalytically active for chemical reactions, in particular, the cleavage or formation of a selected peptide linkage or an ester bond, and which are elicited by such antigens are disclosed as well as methods for producing the antibodies and methods for catalyzing the cleavage or formation of a peptide linkage or in ester bond in a molecule.
    Type: Grant
    Filed: November 2, 1994
    Date of Patent: September 14, 1999
    Assignee: IGEN International Inc.
    Inventors: Michael J. Powell, Richard C. Titmas, Richard J. Massey
  • Patent number: 5952327
    Abstract: Compounds having NEP-inhibitory activity, corresponding to the formula I in whichR.sup.1 is hydrogen or a group forming a biolabile phosphonic acid ester,R.sup.2 is hydrogen or a group forming a biolabile phosphonic acid ester andR.sup.3 is hydrogen or a group forming a biolabile carboxylic acid esterand physiologically acceptable salts of acids of formula I, and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: September 14, 1999
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Harald Waldeck, Joerg Meil, Dirk Thormaehlen, Michael Wurl
  • Patent number: 5945408
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: August 31, 1999
    Assignee: G.D. Searle & Co.
    Inventors: R. Keith Webber, Foe S. Tjoeng, Robert E. Manning
  • Patent number: 5942638
    Abstract: A synthetic process for the selective preparation of reactive polyhedral oligomeric silsesquioxanes (POSS) as well as polyhedral oligomeric silicate (POS) (spherosilicate) is provided. The method claimed herein employs metal catalyzed metathesis reactions for the selective reaction of .alpha.-olefin containing polyhedral oligomeric silsesquioxanes or silicates with olefinic reagents bearing functionalities useful for grafting reactions, polymerization chemistry and sol-gel processes. The use of metal catalyzed metathesis chemistry to form both linear or network polyhedral silsesquioxane polymers directly from .alpha.-olefin-containing polyhedral oligomeric silsesquioxanes is also described.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: August 24, 1999
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Joseph D. Lichtenhan, Joseph J. Schwabb, Frank J. Feher, Daravong Soulivong
  • Patent number: 5939576
    Abstract: A synthetic process for the selective preparation of reactive polyhedral oligomeric silsesquioxanes (POSS) as well as polyhedral oligomeric silicate (POS) (spherosilicate) is provided. The inventive process employs the use of metal catalyzed hydrosilylation reactions for the selective reaction of silane containing polyhedral oligomeric silsesquioxanes or silicates with olefinic reagents bearing functionalities useful for grafting reactions, polymerization chemistry and sol-gel processes. The invention also discloses metal-catalyzed hydrosulfidation reactions and metal-catalyzed hydrophosphidation reacttions for functionalization of polycyclic silicones.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: August 17, 1999
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Joseph D. Lichtenhan, Joseph J. Schwab, Frank J. Feher, Daravong Soulivong